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Non-peptide neuropeptide y antagonists derived from the histamine H2 agonist arpromidine: Role of the guanidine group

1995; Elsevier BV; Volume: 5; Issue: 18 Linguagem: Inglês

10.1016/0960-894x(95)00369-5

1464-3405

Sebastian Knieps, Martin C. Michel, Stefan Dove, Armin Buschauer,

Mast cells and histamine

Abstract Arpromidine analogs in which the guanidino group was replaced or substituted were investigated in functional studies for NPY Y 1 and histamine H 1 antagonism as well as for H 2 agonism (HEL cells, guinea pig ileum and atrium). A basic guanidine or amidine system proved to be important for both Y 1 and H 2 receptor activity. Additional guanidine substitution (Me, cHex, Ph) is compatible with Y 1 antagonism but not with high H 2 agonist potency.